The present invention is concerned with novel substituted .alpha.-fluoromethyl-.alpha.-amino alkanoic acids.
An unsubstituted .alpha.-fluoromethyl-.alpha.-amino alkanoic acid, namely 2-fluoromethylalanine, having the formula: ##STR1## is known [Kollonitsch et al, J. Org. Chem., 40, 3808-9 (1975)]. No specific biological activity for this compound is suggested. This compound (A) is prepared by fluorodehydroxylation of the corresponding 2-hydroxymethylalanine.
.alpha.-Methyl amino acids, such as L-.alpha.-methyl-3,4-dihydroxyphenylalanine (.alpha.-methyldopa, an antihypertensive agent, are known to have decarboxylase inhibiting activity (Goodman, et al., The Pharmacological Basis of Therapeutics, Mac Millan Company, New York, N.Y. 1970, p. 577; Canadian Patent No. 737,907).
Novel substituted .alpha.-fluoromethyl-.alpha.-amino alkanoic acids have been discovered. These novel acids have decarboxylase inhibiting activity significantly greater than that of .alpha.-methyl amino acids.